Dantrium Intravenous
Dantrium Intravenous Uses, Dosage, Side Effects, Food Interaction and all others data.
Dantrium Intravenous has a direct action on skeletal muscle. Dantrium Intravenous depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction.
Dantrium Intravenous is classified as a direct-acting skeletal muscle relaxant. It is currently the only specific and effective treatment for malignant hyperthermia. In isolated nerve-muscle preparation, Dantrium has been shown to produce relaxation by affecting the contractile response of the muscle at a site beyond the myoneural junction. In skeletal muscle, Dantrium dissociates excitation-contraction coupling, probably by interfering with the release of Ca2+ from the sarcoplasmic reticulum. In the anesthetic-induced malignant hyperthermia syndrome, evidence points to an intrinsic abnormality of skeletal muscle tissue. In selected humans, it has been postulated that “triggering agents” (e.g.,general anesthetics and depolarizing neuromuscular blocking agents) produce a change within the cell which results in an elevated myoplasmic calcium. This elevated myoplasmic calcium activates acute cellular catabolic processes that cascade to the malignant hyperthermia crisis. It is hypothesized that addition of Dantrium to the “triggered” malignant hyperthermic muscle cell reestablishes a normal level of ionized calcium in the myoplasm.
Trade Name | Dantrium Intravenous |
Availability | Prescription only |
Generic | Dantrolene |
Dantrolene Other Names | Dantrolene, Dantroleno, Dantrolenum |
Related Drugs | baclofen, Botox, Lioresal, onabotulinumtoxinA, Lyvispah, Dantrium, Ryanodex |
Weight | 20mg, 250mg, 100mg, 25mg, 50mg |
Type | Intravenous powder for injection, oral capsule |
Formula | C14H10N4O5 |
Weight | Average: 314.257 Monoisotopic: 314.065119438 |
Protein binding | Significant, mostly to albumin. |
Groups | Approved, Investigational |
Therapeutic Class | Centrally acting Skeletal Muscle Relaxants |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
In Chronic Spasticity: Dantrium Intravenous is used for controlling the manifestations of clinical spasticity resulting from upper motor neuron disorders (e.g., spinal cord injury, stroke, cerebral palsy or multiple sclerosis). It is of particular benefit to the patient whose functional rehabilitation has been retarded by the sequelae of spasticity. Dantrium Intravenous is not used for the treatment of skeletal muscle spasm resulting from rheumatic disorders.
A decision to continue the administration of Dantrium Intravenous on a long-term basis is justified if introduction of the drug into the patient's regimen:
- Produces a significant reduction in painful and/or disabling spasticity such as clonus, or
- Permits a significant reduction in the intensity and/or degree of nursing care required, or
- Rids the patient of any annoying manifestation of spasticity considered important by the patient himself.
In Malignant Hyperthermia: Oral Dantrium Intravenous is also used preoperatively to prevent or attenuate the development of signs of malignant hyperthermia in known, or strongly suspect, malignant hyperthermia susceptible patients who require anesthesia and/or surgery.
Dantrium Intravenous is also used to associated treatment for these conditions: Malignant Hyperthermia, Spasticity
How Dantrium Intravenous works
Dantrium Intravenous depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction.
Dosage
Dantrium Intravenous dosage
For Use in Chronic Spasticity: It is important that the dosage be titrated and individualized for maximum effect. The lowest dose compatible with optimal response is recommended.Each dosage level should be maintained for seven days to determine the patient’s response. If no further benefit is observed at the next higher dose, dosage should be decreased to the previous lower dose.
Adults: 25 mg once daily for seven days, then 25 mg t.i.d. for seven days, 50 mg t.i.d. for seven days, 100 mg t.i.d.
Pediatric Patients:0.5 mg/kg once daily for seven days, then 0.5 mg/kg t.i.d. for seven days, 1 mg/kg t.i.d. for seven days, 2 mg/kg t.i.d. Therapy with a dose four times daily may be necessary for some individuals. Doses higher than 100 mg four times daily should not be used.
The long-term safety of Dantrium Intravenous in pediatric patients under the age of 5 years has not been established.
For Malignant Hyperthermia:
- Preoperatively: 4 to 8 mg/kg/day of oral Dantrium Intravenous in 3 or 4 divided doses for one or two days prior to surgery, with the last dose being given approximately 3 to 4 hours before scheduled surgery with a minimum of water.
- Post Crisis Follow-up: Oral Dantrium Intravenous should also be administered following a malignant hyperthermia crisis, in doses of 4 to 8 mg/kg per day in four divided doses, for a one to three day period to prevent recurrence of the manifestations of malignant hyperthermia.
Side Effects
The most frequently occurring side effects of Dantrium Intravenous have been drowsiness, dizziness, weakness, general malaise, fatigue, and diarrhea. Other less frequent side effects are constipation, anorexia, abdominal cramps, nausea and/or vomiting, hepatitis, headache, visual disturbance, alteration of taste, insomnia, tachycardia, anemia, leukopenia, lymphocytic lymphoma, mental depression and mental confusion.
Toxicity
Oral LD50 in rats is 7400 mg/kg. Symptoms which may occur in case of overdose include, but are not limited to, muscular weakness and alterations in the state of consciousness (e.g., lethargy, coma), vomiting, diarrhea, and crystalluria.
Precaution
Dantrium Intravenous should be used with caution in patients with impaired pulmonary function, particularly those with obstructive pulmonary disease, and in patients with severely impaired cardiac function due to myocardial disease. Dantrium Intravenous is associated with pleural effusion with associated eosinophilia.
Patients should be cautioned against driving a motor vehicle or participating in hazardous occupations while taking Dantrium Intravenous. Caution should be exercised in the concomitant administration of tranquilizing agents. Dantrium Intravenous might possibly evoke a photosensitivity reaction; patients should be cautioned about exposure to sunlight while taking it.
Interaction
Drowsiness may occur with Dantrium Intravenous therapy and the concomitant administration of CNS depressants such as sedatives and tranquilizing agents may result in further drowsiness. Hepatotoxicity has occurred more often in women over 35 years of age receiving concomitant estrogen therapy. Administration of Dantrium Intravenous may potentiate vecuronium-induced neuromuscular block.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Dantrium Intravenous Drug Interaction
Moderate: diphenhydramine, diphenhydramine, duloxetine, duloxetine, levetiracetam, clonazepam, pregabalin, pregabalin, diazepam, diazepamUnknown: polyethylene glycol 3350, polyethylene glycol 3350, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, ondansetron, ondansetron
Dantrium Intravenous Disease Interaction
Major: hepatotoxicityModerate: cardiac disease, pulmonary impairment
Elimination Route
Bioavailability is 70%.
Half Life
The mean biologic half-life after intravenous administration is variable, between 4 to 8 hours under most experimental conditions, while oral is 8.7 hours for a 100mg dose.
Pregnancy & Breastfeeding use
Pregnancy Category C. Dantrium Intravenous should not be used in nursing mothers.
Contraindication
Active hepatic disease, such as hepatitis and cirrhosis, is a contraindication for use of Dantrium Intravenous.
Acute Overdose
Symptoms: muscular weakness, alterations in the state of consciousness (e.g. lethargy, coma), vomiting, diarrhoea and crystalluria.
Management: Treatment is supportive with ECG monitoring. Admin IV fluids to prevent crystalluria. Maintain an adequate airway and have artificial resuscitation equipment at hand.
Storage Condition
Store between 15-30°C
Innovators Monograph
You find simplified version here Dantrium Intravenous
Dantrium Intravenous contains Dantrolene see full prescribing information from innovator Dantrium Intravenous Monograph, Dantrium Intravenous MSDS, Dantrium Intravenous FDA label